Technetium-99m labelled integrated tropane–BAT as a potential dopamine transporter tracer
[Display omitted] To reduce the molecular weight of 99mTc-labelled tropanes with the aim to enhance the passage over the blood–brain barrier, a so-called integrated tropane–BAT construct was developed. For this purpose a mercaptoethyl substituent was attached to the amine nitrogen atom of a nortropa...
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Veröffentlicht in: | Bioorganic & medicinal chemistry 2005-02, Vol.13 (4), p.1053-1058 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | [Display omitted]
To reduce the molecular weight of
99mTc-labelled tropanes with the aim to enhance the passage over the blood–brain barrier, a so-called integrated tropane–BAT construct was developed. For this purpose a mercaptoethyl substituent was attached to the amine nitrogen atom of a nortropane precursor and the methyl carboxylate in 2β-position was converted to a 2-mercaptoethylaminomethylene substituent. This integrated tropane–BAT construct could be labelled efficiently (85–90%) with technetium-99m. Results of LC–MS analysis of the tracer agent support the assumed structure. Biodistribution studies in normal rats (
n
=
3) showed a slightly higher brain uptake for the new tracer agents as compared to
99mTc-TRODAT-1. These results indicate that further biological evaluation of the integrated
99mTc-tropane–BAT is warranted. |
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ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/j.bmc.2004.11.036 |